EP3784242A4 - Neuartiges verfahren zur herstellung einer phenoxydiaminopyrimidin-verbindung - Google Patents
Neuartiges verfahren zur herstellung einer phenoxydiaminopyrimidin-verbindung Download PDFInfo
- Publication number
- EP3784242A4 EP3784242A4 EP19793313.8A EP19793313A EP3784242A4 EP 3784242 A4 EP3784242 A4 EP 3784242A4 EP 19793313 A EP19793313 A EP 19793313A EP 3784242 A4 EP3784242 A4 EP 3784242A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- synthesis
- novel process
- diaminopyrimidine compound
- phenoxy
- phenoxy diaminopyrimidine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- -1 phenoxy diaminopyrimidine compound Chemical class 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
- C07C37/62—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by introduction of halogen; by substitution of halogen atoms by other halogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
- C07C37/68—Purification; separation; Use of additives, e.g. for stabilisation
- C07C37/70—Purification; separation; Use of additives, e.g. for stabilisation by physical treatment
- C07C37/84—Purification; separation; Use of additives, e.g. for stabilisation by physical treatment by crystallisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/24—Halogenated derivatives
- C07C39/26—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms
- C07C39/27—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms all halogen atoms being bound to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/09—Preparation of ethers by dehydration of compounds containing hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/16—Preparation of ethers by reaction of esters of mineral or organic acids with hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
- C07C41/30—Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862661362P | 2018-04-23 | 2018-04-23 | |
| US201862662991P | 2018-04-26 | 2018-04-26 | |
| PCT/US2019/028014 WO2019209607A1 (en) | 2018-04-23 | 2019-04-18 | Novel process for synthesis of a phenoxy diaminopyrimidine compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP3784242A1 EP3784242A1 (de) | 2021-03-03 |
| EP3784242A4 true EP3784242A4 (de) | 2021-12-22 |
Family
ID=68293586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP19793313.8A Pending EP3784242A4 (de) | 2018-04-23 | 2019-04-18 | Neuartiges verfahren zur herstellung einer phenoxydiaminopyrimidin-verbindung |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11584724B2 (de) |
| EP (1) | EP3784242A4 (de) |
| JP (1) | JP7502997B6 (de) |
| KR (1) | KR20210005592A (de) |
| CN (1) | CN112423756B (de) |
| AU (1) | AU2019257606A1 (de) |
| BR (1) | BR112020020549A8 (de) |
| CA (1) | CA3096505A1 (de) |
| MX (1) | MX2020011258A (de) |
| WO (1) | WO2019209607A1 (de) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2019007163A (es) * | 2016-12-20 | 2019-08-29 | Afferent Pharmaceuticals Inc | Sales cristalinas y polimorfos de un antagonista de p2x3. |
| WO2022060945A1 (en) | 2020-09-17 | 2022-03-24 | Teva Pharmaceuticals International Gmbh | Solid state forms of gefapixant and process for preparation thereof |
| WO2022083476A1 (zh) * | 2020-10-19 | 2022-04-28 | 苏州科睿思制药有限公司 | Gefapixant柠檬酸盐的晶型及其制备方法和用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4422955A (en) * | 1980-12-17 | 1983-12-27 | Sterling Drug Inc. | Process for substitution of aromatic organic compounds |
| WO2008040652A1 (en) * | 2006-10-04 | 2008-04-10 | F. Hoffmann-La Roche Ag | Process for synthesis of phenoxy diaminopyrimidine derivatives |
| WO2018118668A1 (en) * | 2016-12-20 | 2018-06-28 | Afferent Pharmaceuticals, Inc. | Crystalline salts and polymorphs of a p2x3 antagonist |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1725540B1 (de) * | 2004-03-05 | 2012-09-12 | F.Hoffmann-La Roche Ag | Diaminopyrimidine als p2x3- und p2x2/3-antagonisten |
| GB0508422D0 (en) * | 2005-04-26 | 2005-06-01 | Syngenta Ltd | Chemical process |
| CN101253158B (zh) | 2005-09-01 | 2013-07-10 | 弗·哈夫曼-拉罗切有限公司 | 合成芳氧基二氨基嘧啶类化合物的方法 |
| PE20090160A1 (es) * | 2007-03-20 | 2009-02-11 | Wyeth Corp | COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA |
| JP6546592B2 (ja) * | 2013-08-23 | 2019-07-17 | アファレント ファーマシューティカルズ インコーポレイテッド | 急性、亜急性または慢性の咳を治療するためのジアミノピリミジンｐ２ｘ３およびｐ２ｘ２／３受容体モジュレーター |
-
2019
- 2019-04-18 CN CN201980027166.3A patent/CN112423756B/zh active Active
- 2019-04-18 US US17/048,833 patent/US11584724B2/en active Active
- 2019-04-18 JP JP2020560241A patent/JP7502997B6/ja active Active
- 2019-04-18 BR BR112020020549A patent/BR112020020549A8/pt unknown
- 2019-04-18 MX MX2020011258A patent/MX2020011258A/es unknown
- 2019-04-18 CA CA3096505A patent/CA3096505A1/en active Pending
- 2019-04-18 KR KR1020207030049A patent/KR20210005592A/ko not_active Application Discontinuation
- 2019-04-18 WO PCT/US2019/028014 patent/WO2019209607A1/en active Application Filing
- 2019-04-18 EP EP19793313.8A patent/EP3784242A4/de active Pending
- 2019-04-18 AU AU2019257606A patent/AU2019257606A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4422955A (en) * | 1980-12-17 | 1983-12-27 | Sterling Drug Inc. | Process for substitution of aromatic organic compounds |
| WO2008040652A1 (en) * | 2006-10-04 | 2008-04-10 | F. Hoffmann-La Roche Ag | Process for synthesis of phenoxy diaminopyrimidine derivatives |
| WO2018118668A1 (en) * | 2016-12-20 | 2018-06-28 | Afferent Pharmaceuticals, Inc. | Crystalline salts and polymorphs of a p2x3 antagonist |
Non-Patent Citations (4)
| Title |
|---|
| GUO WEN-SHENG ET AL: "Cocrystal Phenomena of DABCO with Phenol Derivatives", CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, VOL.9, N°.3 (1993), 1 January 1993 (1993-01-01), pages 261 - 263, XP055859768, Retrieved from the Internet <URL:http://crcu.jlu.edu.cn/EN/Y1993/V9/I3/261> [retrieved on 20211110] * |
| MINO R CAIRA ED - MONTCHAMP JEAN-LUC: "Crystalline Polymorphism of Organic Compounds", TOPICS IN CURRENT CHEMISTRY; [TOPICS IN CURRENT CHEMISTRY], SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP008166276, ISSN: 0340-1022, [retrieved on 19990226], DOI: 10.1007/3-540-69178-2_5 * |
| NAOKI TAKAHASHI ET AL: "Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists", BIOORGANIC, vol. 22, no. 1, 1 January 2014 (2014-01-01), AMSTERDAM, NL, pages 488 - 498, XP055219666, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2013.11.001 * |
| See also references of WO2019209607A1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US11584724B2 (en) | 2023-02-21 |
| EP3784242A1 (de) | 2021-03-03 |
| MX2020011258A (es) | 2021-01-20 |
| JP7502997B6 (ja) | 2024-07-12 |
| CN112423756A (zh) | 2021-02-26 |
| WO2019209607A1 (en) | 2019-10-31 |
| US20210122717A1 (en) | 2021-04-29 |
| BR112020020549A2 (pt) | 2021-01-12 |
| AU2019257606A1 (en) | 2020-10-01 |
| CN112423756B (zh) | 2024-08-13 |
| CA3096505A1 (en) | 2019-10-31 |
| JP2021523886A (ja) | 2021-09-09 |
| BR112020020549A8 (pt) | 2023-02-07 |
| JP7502997B2 (ja) | 2024-06-19 |
| KR20210005592A (ko) | 2021-01-14 |
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Legal Events
| Date | Code | Title | Description |
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| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE |
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| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE |
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| PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
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| STAA | Information on the status of an ep patent application or granted ep patent |
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| 17P | Request for examination filed |
Effective date: 20201123 |
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| AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR |
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| AX | Request for extension of the european patent |
Extension state: BA ME |
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| DAV | Request for validation of the european patent (deleted) | ||
| DAX | Request for extension of the european patent (deleted) | ||
| A4 | Supplementary search report drawn up and despatched |
Effective date: 20211119 |
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| RIC1 | Information provided on ipc code assigned before grant |
Ipc: C07D 239/48 20060101ALI20211115BHEP Ipc: C07C 253/30 20060101ALI20211115BHEP Ipc: C07D 487/08 20060101ALI20211115BHEP Ipc: C07C 37/84 20060101ALI20211115BHEP Ipc: C07C 37/62 20060101ALI20211115BHEP Ipc: A61K 31/505 20060101AFI20211115BHEP |
|
| RAP1 | Party data changed (applicant data changed or rights of an application transferred) |
Owner name: WERTHENSTEIN BIOPHARMA GMBH Owner name: MERCK SHARP & DOHME LLC |
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| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: EXAMINATION IS IN PROGRESS |
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| 17Q | First examination report despatched |
Effective date: 20240507 |